module 4 anti-rheumatic drugs Flashcards
drugs for osteoarthritis
analgesia - APAP - NSAIDS - COX-2 inhibitors inflammation if present - NSAIDS - COX-2 inhibitors - intra-articular corticosteroids
rheumatoid arthritis drugs
ASA at inflammatory doses: rarely used d/t AE
symptomatic therapy
- NSAID
- corticosteroids- systemic, intra-articular
Prevent or slow progression
- DMARDs
corticosteroid use
anti-inflammatory life-threatening complication of RA: - vasculitis bridge time to onset of DMARD pulse therapy for acute flare ups intra-articular therapy for acute inflammation
Corticosteroid AE
hyperglycemia cataracts glaucoma aseptic necrosis of weight bearing joints osteoporosis cushing syndrome adrenal suppression Na and H2O retention CNS side effects
corticosteroids with mineralcorticoid activity
cortisone
hydrocortisone
prednisone
prednisolone
mineralcorticoid activity
promotes Na/H2O retention
Disease modifying antirheumatic drugs (DMARDs)
standard of care
ideally used when Dx of RA is established
prevent or slow progression of joint destruction
- relatively toxic, potent, very expensive
conventional DMARD drugs
hydroxychloroquine methotrexate azathioprine gold penicillamine sulfasalazine leflunomide minocycline cyclophosphamide
biologic DMARDs
etanercept infliximab adalimumab certolizumab golimumab tocilizumab rituximab abatacept anakinra
DMARD monitoring
may take 3-6mo for response
response is often incomplete
- continue NSAID
Monitor ROM, ADL
DMARD seldom used and their AE
gold, penicillamine
- high toxicity
- myelosuppression
- proteinuria
- stomatitis
- rash
- altered taste
- visual changes
Azathioprine (PO)
also for crohn’s disease
prodrug for mercaptopurine
immunosuppressant
reserved for aggressive disease or serious complications
azathioprine AE
myelosuppression
hepatotoxicity
rash
infection
hydroxychloroquine (PO)
primarily for mild RA
also an antimalarial drug
hydroxychloroquine AE
some GI upset
retinopathy: rare
- eye exam every 6-12 months
sulfasalazine (PO)
mild to moderate RA
also for crohn’s and UC
becomes: sulfapyridine and 5-aminosalicylic acid in intestine
sulfasalazine AE
GI upset
rash
bodily fluids can turn yellow-orange
can bind to iron and dec. absorption
sulfasalazine precaution
pt on antibiotic; intestinal flora may be destroyed, reducing conversion to active form.
leflunomide (PO) MOA
inhibitor of pyrimidine synthesis
-> altered lymphocyte activation and dec. inflammatory response
leflunomide AE
hepatotoxicity reversible alopecia GI distress Preg: X -- cholestyramine can quickly lower drug levels in pts who wish to become pregnant
Methotrexate (PO, IM, subQ) MOA
folate antagonist -> purine biosynthesis inhibition, cytokine production inhibition, adenosine production stimulation -> anti-inflammatory effect
methotrexate AE
GI upset
megaloblastic anemia
- pt should receive folic acid replacement
hepatotoxicity
Biologic DMARD advantage
no routine laboratory monitoring
biologic DMARD disadvangates
risk of infections and malignancy
- temp. suspend tx if occur
very expensive
Parenteral: injection site reactions common
Biologic DMARDs: TNF-a blocker drugs
etanercept infliximab adalimumab certolizumab pegol golimumab - may use in combo with DMARD
biologic DMARD MOA
downregulate or antagonize TNF-a, a key cytokine in RA
biologic DMARD AE
infections
- fungal infections
- active TB, and reactivation of latent TB
- bacterial infection
- viral infection
- opportunistic infections
lymphoma and other malignancies in children and teens
Rituximab (biologic DMARD)
depletes B-cells which have been shown to be responsible for inflammation in RA
- use when pt fails traditional DMARD and anti-TNF agents
rituximab AE
fatal infusion reactions
severe mucocutaneous reactions
PML
Abatacept (biologic DMARD)
inhibits T cell activation
- use when pt fails traditional DMARD and anti-TNF
anakinra (biological DMARD)
antagonized IL-1 receptors, a proinflammatory cytokine
- use when pt fails traditional DMARD and anti-TNF
- can use in combo with DMARD but not other anti-TNF
tocilizumab (biologic DMARD)
inhibits IL-6
use when patient fail anti-TNF drugs
tocilizumab AE
serious risk of infections
- invasive fungal infection
- active TB, and reactivation of latent TB
- bacterial infection
- viral infection
- opportunistic infections
methotrexate benefits
cheap
well tolerated
take effect within one month
- most commonly used DMARD
